2POB

PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709

2POB の概要

• エントリーDOI: 10.2210/pdb2pob/pdb
• 分子名称: Peroxisome proliferator-activated receptor gamma, N-[(2S)-2-[(2-BENZOYLPHENYL)AMINO]-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL]ACETAMIDE, GLYCEROL, ... (4 entities in total)
• 機能のキーワード: pparg, nuclear receptor, ppar, gene regulation
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus: P37231
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 62854.04

構造登録者

Nolte, R.T. (登録日: 2007-04-26, 公開日: 2008-03-18, 最終更新日: 2024-04-03)

主引用文献

Trump, R.P.,Cobb, J.E.,Shearer, B.G.,Lambert, M.H.,Nolte, R.T.,Willson, T.M.,Buckholtz, R.G.,Zhao, S.M.,Leesnitzer, L.M.,Iannone, M.A.,Pearce, K.H.,Billin, A.N.,Hoekstra, W.J.
Cocrystal structure guided array synthesis of PPARgamma inverse agonists
BIOORG.MED.CHEM.LETT., 17:3916-3920, 2007

PubMed Abstract: PPARgamma-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARgamma rich adipose. Both pro- and anti-adipogenic PPARgamma ligands promote glucose and lipid lowering in animal models of diabetes. Herein, we disclose representatives of an array of 160 farglitazar analogues with atypical inverse agonism of PPARgamma in mature adipocytes.

PubMed: 17533125
DOI: 10.1016/j.bmcl.2007.04.111

実験手法

X-RAY DIFFRACTION (2.3 Å)